Table 2. Effect of R1 on Human GPR139 Potency.
| Cmpd | R1 | EC50 (nM)a | Emax (%)b |
|---|---|---|---|
| 7a | H | 162 ± 30 | 130 |
| 7b | 2-Cl | 150 ± 23 | 120 |
| 7c | 3-Cl | 16 ± 2 | 138 |
| 7d | 4-Cl | 118 ± 49 | 117 |
| 7e | 3-Me | 24 ± 5 | 137 |
| 7f | 3-CN | 59 ± 13 | 129 |
| 7g | 3-F | 54 ± 11 | 118 |
| 7h | 3-MeO | 33 ± 7 | 146 |
| 7i | 3-CF3 | 52 ± 17 | 134 |
| 7j | 3-OCF3 | 46 ± 22 | 129 |
| 7k | 2,3-diCl | 52 ± 21 | 113 |
| 7l | 3,4-diCl | 193 ± 76 | 106 |
| 7m | 2,5-diCl | 40 ± 14 | 139 |
| 7n | 3,5-diCl | 46 ± 4 | 119 |
| 7o | 3-Cl,5-F | 24 ± 22 | 124 |
| 7p | 3-Br, 5-Cl | 78 ± 8 | 113 |
| 7q | 3,5-diMeO | 32 ± 7 | 149 |
| 8 | >10 000 | ND | |
| 9 | >10 000 | ND | |
| 1 | 43 | 125 |
a
Data are reported as mean ± SEM from at least three experiments.
b
The efficacy of l-Trp was set to 100%.